Beta Lactam penicillin Flashcards by joseph dizon

The peptidoglycan is composed of glycan chains, which are linear strands of two alternating amino sugars

Nag Nam

N-acetylglucosamine and N-acetylmuramic acid

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First stage of peptidoglycan biosynthesis

precursor formation
uridine diphosphate (UDP)acetylmuramyl-pentapeptide
Park neucleotide

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Second stage of peptidoglycan biosynthesis

UDP-acetylmuramylpentapeptide and UDPacetylglucosamine

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Third stage of biosynthesis of peptidoglycan

transpeptidation reaction

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Last step in peptidoglycansynthesis

Inhibited by beta lactam antibiotics

By inhibiting the enzyme transpeptidase

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Penicillins as well as cephalosporins are called beta-lactam antibiotics and are characterized by threefundamental structural requirements

Beta lactam structure
Carboxyl acid group
Amino acid side chains

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The lactam structure can also be viewed as the covalent bonding of pieces of two amino acids

Cysteine and valine

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The compound consists of 2 basic structures of penicillin

Thiazolidine Ring

2. Beta-Lactam Ring

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the parent compound of all semisynthetic penicillins

6 amino penicillinic acid

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Gram negative cocci

Moraxella catarrhalis
Neisseria gonorrheae
Neisseria meningitidis

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Gram positive cocci

Streptococcus pneumoniae 
Streptococcus, hemolytis (A,B,C,D) 
Streptococcus viridans 
Staphylococcus aureus 
Enteroccocus faecalis 
Enteroccocus faecium

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Gram positive rods

Actinomycoses
Bacillus Clostridium
Corynebacterium diphtheriae/jeikeium
Listeria

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Acid-‐fast rods

Mycobacterium

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Spirochetes

Borrelia bugdorferi/recurrentis,
Leptospira,
Treponema pallidium/pertenue

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Chlamydiae

psittaci,
trachomatis,
pneumoniae

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Penicillin greatest activity with

gram-positive organisms,
gram negative cocci,
non-beta lactamase producing anaerobes

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Penicillin little activity against

gram-negative rods

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Pencillin Susceptible to destruction/hydrolysis by

Beta lactamase

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Narrow spectrum penicillin

Benzylpenicillin –Penicillin G 
•High activity against gram  (+) 
•Low activity against gram -
Phenoxymethyl penicillin-Penicillin V 
•Oral penicillin

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Extended spectrum penicillin

Amino penicillins
Carboxy penicillin
Ureido penicillin

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Aminopenicillins

Ampicillin

a. 2 Esters
a. 2.1. Bacampicillin
a. 2.2. Pivampicillin
a. 2.3. Talampicillin
a. 3. Amoxicillin

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Carboxy penicillins

Carbenicillin                   
b.1.1  Indanyl Carbenicillin     
b 1.2  Disodium Carbenicillin       
b.2     Ticarcillin 
b.3     Temocillin

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Ureido penicillin

Mezlocillin

c. 2. Azlocillin
c. 3. Piperacillin
c. 4. Apalcillin

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CARBOXYPENICILLINS and UREIDOPENICILLINS

Pseudomonas aeruginosa-‐

Bacteroides fragilis

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Carboxypenicillins

Certain indole - proteus

Ureidopenicillins

Klebsiella

First antipseudomonal carboxypenicillin Obsolete: CHF, hypoK+, abnormal platelet aggregation

Carbenicillin

derivative use in UTI

Carbenicillin indanyl Na

Less active than ampicillin against enterococci | –Pseudomonas but inferior to piperacillin and mezlocillin

Ticarcillin

more active in Klebsiella; Pseudomonas; Enterococcus faecalis

Mezlocillin

Pseudomonas; Enterobacteriaceae; many Bacteroides

Piperacillin

retain antibacterial spectrum of penicillin •improved activity against gram (-) organisms •destroyed by beta-lactamases

Ampicillin and Antipseudomonal Penicillins

resistant to staphylococcal beta-lactamases active against staphylococci and streptococci inactive against enterococci & anaerobic bacteria, and gramnegative cocci & rods

Antistaphylococcal penicillins(Penicillinaseresistant

Methicillin (Staphcillin) Nafcillin ( Unipen, Nafcil, Nallpen) Isoxazolyl penicillins a. Oxacillinb. Dicloxacillin c. Cloxacillind. Flucloxacillin

resistant to staphylococcal beta-lactamases •active to staphylococci and streptococci •Not active against enterococci, anaerobic bacteria and gram –cocci and rods

Nafcillin

not suitable for oral administration

Nafcillin

Acid stable

Dicloxacillin, Amoxicillin, Ampicillin

can inhibit transfer from CSF to blood stream (pen)

Probenecid

biliary excretion

Nafcillin

kidney & biliary excretion

Oxacillin, dicloxacillin, cloxacillin

Repository preparation of pen G

penicillin Gprocaine (4 to 5 days) | penicillin G benzathine (26 days

inadvisable particularly with benzylpenicillin as it can cause convulsions

Intratechal administration

5-‐10x less active against gram (-‐) microbes, esp. Neisseria and certain anaerobes better absorbed from the GIT

Pen V

oral form in minor infections relative poor bioavailability; dosing 4x a day Narrow antibacterial spectrum

most active of the oral beta lactamsvspen resistant pneumococcistrains

Amoxicillin and ampicillin

effective for shigellosis

Ampicillin

Extended spectrum penicillin that have better absorption

Amoxicillin

not used to treat uncomplicated salmonella gastroenteritis somewhat less active than Pen G vs gram (+) cocci enterococcal grp. D and viridans grp of streptococci Listeria monocytogenes H. influenza. And E. coli

Ampi and amoxicillin

no longer used bec. of its nephrotoxicity

Methicillin

Adverse effect

Hypersensitivity reactions Gastrointestinal disturbances after oral administration 3. Convulsions following rapid IV injection 4. Accidental injection to sciatic nerve 5. Hepatitis

pulmonary embolism -acute psychotic reactions AE

Procaine pen G after accidental injection

hepatitis -granulocytopenia, bone marrow depression AE

Oxacillin and nafcillin

Hypernatremia AE

Disodium Carbenicillin and high dose Penicillin G Na

hyperkalemia with high doses AE

Pen G K

Jarisch-Herxheimerreaction AE

Pen G Na

bleeding diathesis AE

Carbenicillinand Ticarcillin

interstitial nephritis AE

Methicillin

pseudomembranous colitis AE

Ampicillin

Penicillinsbindtoandinactivateaminoglycosides

Chemical antagonism

Penicillin G and its close congener penicillin V are highly active against

gram-positive cocci, but they are readily hydrolyzed by penicillinase

ineffective against most strains of Staphylococcus aureus

Pen G and Pen V

The penicillinase-resistant penicillins (methicillin, nafcillin, oxacillin, cloxacillin, and dicloxacillin) have less potent antimicrobial activity against

microorganisms that are sensitive to penicillin G | effective against penicillinase-producing Staph. aureus

Ampicillin, amoxicillin, bacampicillin, and others comprise a group of penicillins whose antimicrobial activity is extended to include such

gram-negative microorganisms as Haemophilus influenzae, E. coli, and Proteus mirabilis

DOC for meningitis; pneumococcal pneumonia and pneumococcal meningitis

Penicillin G (benzylpenicillin

most penicillin-‐resistant pneumococci are resistant to

3rd generation cephalosporin

Penicillin G -‐resistant to

S. aureus, S. epidermidis, Strep. viridans, Corynebacterium diphtheria

Endocarditis ( Strep. viridans

Procaine Pen G Pen G plus Streptomycin or gentamycin

Enterococci endocarditis

Pen G + aminoglycosides

Syphilis

Pen G procaine + probenecid

Actinomycosis

Pen G + oral pen V

Diphtheria (eliminate carrier

Pen G procaine injection (single)

Gingivostomatitis

Pen V

Anthrax Clostridial Erysipelas Endocarditis

Pen G

Lyme disease

Tetracycline | Amoxicillin

heteropolymeric component of the cell wall that provides rigid mechanical stability by virtue of its highly cross-linked latticework structure

Peptidoglycan